Convenient access both to highly antimalaria-active 10-arylaminoartemisinins, and to 10-alkyl ethers including artemether, arteether, and artelinate |
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Authors: | Haynes Richard K Chan Ho-Wai Ho Wing-Yan Ko Cliff Ki-Fung Gerena Lucia Kyle Dennis E Peters Wallace Robinson Brian L |
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Affiliation: | Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, PR China. haynes@ust.hk |
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Abstract: | An economical phase-transfer method is used to prepare 10-arylaminoartemisinins from DHA and arylamines, and artemether, arteether, and artelinate from the corresponding alcohols. In vivo sc screens against Plasmodium berghei and P. yoelii in mice reveal that the p-fluorophenylamino derivative 5 g is some 13 and 70 times, respectively, more active than artesunate; this reflects the very high sc activity of 10-alkylaminoartemisinins. However, through the po route, the compounds are less active than the alkylaminoartemisinins, but still approximately equipotent with artesunate. |
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Keywords: | antimalarial artemisinin glycosylamine phase‐transfer catalysis synthesis |
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